目录号 | 产品详情 | 靶点 | |
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T40650 | |||
Dihydroisopimaric acid activates BK channels alphabeta1, which are large conductance Ca 2+ activated K + channels. This compound directly measures the opening of BKalphabeta1 under a whole-cell voltage clamp. | |||
T33407 | |||
MitoEbselen-2 is a radiation mitigator which reduces lipid hydroperoxides and prevents apoptotic cell death. When administered 24 hours postirradiation, MitoEbselen-2 was shown to increase the survival of mice exposed to whole body γ-irradiation. | |||
T38266 | |||
Potent γ-secretase inhibitor (IC50 values are 1.2 and 6.2 nM in whole cell and cell-free assays, respectively). Reduces Aβ in brain, CSF and plasma in mice and guinea pigs. Lanz et al (2010) Pharmacodynamics and pharmacokinetics of the gamma-secretase inhibitor PF-3084014. J.Pharmacol.Exp.Ther. 334 269 PMID:20363853 | |||
T37763 | |||
Selective TRPC5 activator (EC50 = 1.4 μM in a calcium influx assay, 1.3 μM in whole cell patch clamp assay). Displays >14.5-fold selectivity for TRPC5 over other TRP channels (EC50 = 20.6 μM for TRPM8). Also activates TRPC1:5 and TRPC4:5 heteromers. Beckmann et al (2017) A benzothiadiazine derivative and methylprednisolone are novel and selective activators of transient receptor potential canonical 5 (TRPC5) channels. Cell Calcium. 66 10 PMID:28807145 | |||
T83326 | |||
4-Acetamido-4'-isothiocyanatostilbene-2,2'-disulfonic acid disodium 是荧光染料,用于逆行轴突运输二抗标记显示和全细胞荧光染色。 | |||
T41212 | |||
FTI 277 is a prodrug form of FTI 276 that inhibits farnesyltransferase (FTase) (IC50 = 0.5 nM). Inhibits H-Ras and K-Ras processing in whole cells (IC50 values are 0.1 and 10μM respectively) and disrupts constitutive H-Ras-specific activation of MAPK. Causes significant antiproliferative effects in human malignant glioma cells and many other tumor cell lines. | |||
T26447 | |||
A 78773 is a potent, selective, direct, and reversible 5-lipoxygenase inhibitor. It has activity in a variety of purified cells and in more complex biological systems such as whole blood, lung fragments, and tracheal tissues. A 78773 acts against inflamma | |||
T26865 | |||
BMS-933043 is a Selective α7 nAChR partial agonist. BMS-933043 showed potent binding affinity to native rat (Ki = 3.3 nM) and recombinant human alpha7 nicotinic acetylcholine receptors (Ki = 8.1 nM). BMS-933043 shows agonist activity in a calcium fluoresc | |||
T80455 | Sodium Channel | ||
ω-Conotoxin CVIB为非选择性N型及P/Q型电压门控钙通道(VGCC)拮抗剂,能够抑制背根神经节(DRG)中神经元去极化后激活全细胞VGCC电流,其pIC50值为7.64。 | |||
T63405 | |||
NAZ2329 是受体型蛋白质酪氨酸磷酸酶 (RPTPs) R5 亚家族的一个细胞可渗透抑制剂,与其他 PTPs 相比,其变构且能够优先抑制 PTPRZ (hPTPRZ1 的IC50= 7.5 μM) 和PTPRG (hPTPRGIC50= 4.8 μM)。NAZ2329 能够与PTPRZ 的 D1结构域结合,与PTPRZ 整个 (D1 + D2) 片段相比,其能够更有效地抑制 PTPRZ1-D1片段 (IC50: 1.1 μM)。NAZ2329 能够抑制胶质母细胞瘤细胞的肿瘤生长,并表现出抑制干细胞样特性。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-02306 | MAB21L2 Protein, Human, Recombinant (His & ZZ) | Human | E. coli | ||
MAB21L2 (Mab-21 Like 2) is a Protein Coding gene. It encodes a protein similar to C. elegans mab-21 cell fate-determining factor. The protein encoded by this gene is primarily nuclear, although some cytoplasmic localization has been observed. MAB21L2 belongs to the mab-21 family. It is required for several aspects of embryonic development including normal development of the eye. It is thought that this gene may also be involved in neural development. The identification of MAB21L2 as a novel factor involved in human coloboma and highlight the power of genome editing manipulation in model organisms for analysis of the effects of whole-exome variation in humans. Diseases associated with MAB21L2 include Microphthalmia/Coloboma And Skeletal Dysplasia Syndrome and Microphthalmia.
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TMPH-03741 | BoNT/F Protein, Clostridium botulinum, Recombinant (His) | Clostridium botulinum | E. coli | ||
Botulinum toxin causes flaccid paralysis by inhibiting neurotransmitter (acetylcholine) release from the presynaptic membranes of nerve terminals of the eukaryotic host skeletal and autonomic nervous system, with frequent heart or respiratory failure. Precursor of botulinum neurotoxin F which may have 2 coreceptors; complex polysialylated gangliosides found on neural tissue and specific membrane-anchored proteins found in synaptic vesicles. Receptor proteins are exposed on host presynaptic cell membrane during neurotransmitter release, when the toxin heavy chain (HC) binds to them. Upon synaptic vesicle recycling the toxin is taken up via the endocytic pathway. When the pH of the toxin-containing endosome drops a structural rearrangement occurs so that the N-terminus of the HC forms pores that allows the light chain (LC) to translocate into the cytosol. Once in the cytosol the disulfide bond linking the 2 subunits is reduced and LC cleaves its target protein on synaptic vesicles, preventing their fusion with the cytoplasmic membrane and thus neurotransmitter release. Whole toxin only has protease activity after reduction, which releases LC. Requires complex eukaryotic host polysialogangliosides for full neurotoxicity. It is not clear whether a synaptic vesicle protein acts as its receptor; there is evidence for and against SV2 fulfilling this function.; Has proteolytic activity. After translocation into the eukaryotic host cytosol, inhibits neurotransmitter release by acting as a zinc endopeptidase that catalyzes the hydrolysis of the '60-Gln-|-Lys-61' bond of synaptobrevin-1/VAMP1 and the equivalent 'Gln-|-Lys' sites in VAMP2 and VAMP3. Cleaves the '48-Gln-|-Lys-49' bond of A.californica synaptobrevin (AC P35589).; Responsible for host epithelial cell transcytosis, host nerve cell targeting and translocation of light chain (LC) into host cytosol. Composed of 3 subdomains; the translocation domain (TD), and N-terminus and C-terminus of the receptor-binding domain (RBD). The RBD is responsible for the adherence of the toxin to the cell surface. It simultaneously recognizes 2 coreceptors; polysialated gangliosides and the receptor protein SV2A, SV2B and SV2C in close proximity on host synaptic vesicles; although not all evidence indicates these are the receptors. The N-terminus of the TD wraps an extended belt around the perimeter of the LC, protecting Zn(2+) in the active site; it may also prevent premature LC dissociation from the translocation channel and protect toxin prior to translocation. The TD inserts into synaptic vesicle membrane to allow translocation into the host cytosol.
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